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Chem Cent J. 2017 Aug 08;11(1):80. doi: 10.1186/s13065-017-0312-2.

Bis-pyrimidine acetamides: design, synthesis and biological evaluation.

Chemistry Central journal

Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Mani Vasudevan, Syed Adnan Ali Shah, Balasubramanian Narasimhan

Affiliations

  1. Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
  2. Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
  3. Collaborative Drug Discovery Research (CDDR) Group, Pharmaceutical Life Sciences Community of Research, Universiti Teknologi MARA (UiTM), 40450, Shah Alam, Selangor Darul Ehsan, Malaysia.
  4. Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Buraidah, 51452, Kingdom of Saudi Arabia.
  5. Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA, Puncak Alam Campus, 42300, Bandar Puncak Alam, Selangor D. E, Malaysia.
  6. Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India. [email protected].

PMID: 29086907 PMCID: PMC5548699 DOI: 10.1186/s13065-017-0312-2

Abstract

BACKGROUND: In the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine acetamides by Claisen-Schmidt condensation and screened for its in vitro antimicrobial and anticancer activities.

RESULTS: The synthesized bis-pyrimidine acetamide derivatives were confirmed by IR,

CONCLUSIONS: The biological study demonstrated that compounds 3, 13, 16, 17 and 18 were found to be most active antimicrobial agents with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compounds 12, 16 and 18 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line with best IC

Keywords: Anticancer; Antimicrobial; Bis-pyrimidines; Claisen–Schmidt condensation; SAR

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